Aim: To evaluate the cytotoxic activity of newly synthesized a series of novel HDAC inhibitors comprising sulfonamide as zinc binding group and Isatin derivatives as cap group joined by mono amide linker as required to act as HDAC inhibitors. Materials and Methods: The utilization of sulfonamide as zinc binding group joined by N-alkylation reaction with ethyl-bromo hexanoate as linker group that joined by amide reaction with Isatin derivatives as cap groups which known to possess antitumor activity in the designed of new histone deacetylase inhibitors and using the docking and MTT assay to evaluate the compounds. Results: Four compounds have been synthesized and characterized successfully by ART-FTIR, NMR and ESI-Ms. the compounds were synthesized and characterized by successfully by ART-FTIR, NMR and ESI- Ms. Assessed for their cytotoxic activity against human colon adenocarcinoma MCF-7 (IC50, I=105.15, II=60.00, III=54.11, IV=56.57, vorinostat=28.41) and hepatoblastoma HepG2 (IC50, I=63.91, II=135.18, III=118.85, IV=51.46, vorinostat=37.50). Most of them exhibited potent HDAC inhibitory activity and significant cytotoxicity. Conclusions: The synthesized compounds (I, II, III and IV) showed cytotoxicity toward MCF-7 and HepG2 cancer cell lines and their docking analysis provided a preliminary indication that they are viable [HDAC6] candidates.
The present work involved four steps: First step include reaction of acrylamide ,N-?-Methylen-bis(acryl amide) and N-tert Butyl acryl amide with poly acryloyl chloride in the presence of triethyl amine (Et3N) as catalyst, the second step include homopolymerization of all products of the first step by using benzoyl peroxide(BPO) as initiator in (80-90)Co in the presence of Nitrogen gas(N2). In the third step the poly acrylimide which prepare in second step was convert into potassium salt by using alcoholic potassium hydroxide solution. Fourth step include Alkylation of the prepared polymeric salts in third step by react it with different alkyl halides(benzyl chloride, allylbromide , methyl iodide) by using DMF as solvent for(10-12) hours.
... Show Morefour coordinated complexes for divalent metal ions : Mn, Fe, Co, Ni, Cu and Cd have been synthesized using bidentate Schiff base ligand type (NN)formed by the condensation of o-phenylenediamine , p- methylbenzadehyde and furfural in methanol. The ligand was reacted with divalent metal chloride forming complexes of the types :[M(L)Cl2] where : MII=Mn, Fe, Ni, Cu, and Cd . These new compounds were characterized by elemental analysis, spectroscopic methods (FT-IR, U.V-Vis, 1HNMR (for ligand only and atomic absorption) , magnetic susceptibility, chloride content along with conductivity measurement. These studies revealed that the geometry for all complexes about central metal ion is tetrahedral.
This research was conduct to evaluate the cytotoxic effect of exotoxin A (ETA) produced by Pseudomonas aeruginosa on mice in comparison with (phosphate buffer saline (PBS) as a negative control. The effect of the toxin was measured by employing the cytogenetic analysis which included (the mitotic index (MI), chromosomal aberrations (CAs), micronucleus (MN) and sperm abnormalities) parameters. In order to specify the cytotoxic effect of the toxin, three doses of ETA (125, 250 and 500 ng/ml) were used. Results showed that ETA was found to cause a significant decrease in mitotic index (MI) percentage, while significant increase in micronucleus (MN), chromosomal aberrations (CAs) and sperm abnormalities parameters in compression with control wa
... Show MoreThis research work aims to the determination of molybdenum (VI) ion via the formation of peroxy molybdenum compounds which has red-brown colour with absorbance wave length at 455nm for the system of ammonia solution-hydrogen peroxide-molybdenum (VI) using a completely newly developed microphotometer based on the ON-Line measurement. Variation of responses expressed in millivolt. A correlation coefficient of 0.9925 for the range of 2.5-150 ?g.ml-1 with percentage linearity of 98.50%. A detection limit of 0.25 ?g.ml-1 was obtained. All physical and chemical variable were optimized interferences of cation and anion were studied classical method of measurement were done and compared well with newly on-line measurements. Application for the use
... Show MoreTwelve N-(6-sustirured benzothanol-2-y1) succinamic acids and 3-(6-substitted benzonathol-2-y1)-carbamoyl propionyl chloride were synthesized in good yields from reaction of benzonathol2-yl)
Asthma is a chronic respiratory disorder of airways characterized by inflammation, hyperresponsiveness, inflammatory cell infiltration, mucous secretion, and remodelling. Ammi majus is medicinal plant belong to family of Apiaceous which has anti-inflammatory and antioxidant activities. This study designed to investigate of anti-asthmatic activity of alcoholic extract of Ammi majus in improvement of asthma. Forty-eight healthy female mice divided to six groups Group I: the negative control group (distal water only), Group II: Positive control group (ovalbumin group), Group III: Ammi majus (64 mg/kg/day) with sensitization, Group IV:Ammi majus (128 mg/kg/day) w
... Show MoreAsthma is a chronic respiratory disorder of airways characterized by inflammation, hyperresponsiveness, inflammatory cell infiltration, mucous secretion, and remodelling. Ammi majus is medicinal plant belong to family of Apiaceous which has anti-inflammatory and antioxidant activities. This study designed to investigate of anti-asthmatic activity of alcoholic extract of Ammi majus in improvement of asthma. Forty-eight healthy female mice divided to six groups Group I: the negative control group (distal water only), Group II: Positive control group (ovalbumin group), Group III: Ammi majus (64 mg/kg/day) with sensitization, Group IV:Ammi majus (128 mg/kg/day) with sensitization, Group V: Ammi majus (64 mg/kg/day) without sensitiza
... Show MoreA new ligand complexes have been synthesis from reaction of metal ions of MnII , CoII , NiII , CuII , ZnII , CdII and PdII with schiff base [(E)-1-((2-amino-5-(3, 4, 5-trimethoxybenzyl) pyrimidin-4-ylimino) methyl) naphthalen-2-ol [HL)]. The prepared [HL] was characterized by FT-IR, UV-Vis spectroscopy, 1H13CNMR spectra Mass spectra and melting point. The compounds were characterized by techniques UV-Vis and FT-IR spectral studies, micro analysis (C.H.N), determination of atomic absorption, chloride content, molar conductivity measurements, magnetic susceptibility and melting point. The ligand acts as a monobasic tridentate, coordinating through deprotonated phenolic O and azomethine N atoms. The compounds are neutral electrolytic in dimeth
... Show MoreA crucial area of research in nanotechnology is the formation of environmentally benign nanoparticles. Both unicellular and multicellular play an important role in synthesis nanoparticles through the production of inorganic materials either intracellularly or extracellularly. The agents (pigments, siderophores, cell extracted metabolites and reducing compounds) were used to prepare silver nanparticles with different sizes and shapes. The color variations (dark yellow, slightly dark yellow and golden yellow) arising from changes in the composition, size, and shape of nanoparticles, surrounding medium can be monitored using UV-visible spectrophotometer. These effects are due to the phenomena called surface plasmon resonance. The silver nanopa
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